Instructions for use BEROTEK (BEROTEC)
Suction
Depending on the method of inhalation and the inhalation system used, about 10-30% of the active substance released from the aerosol preparation after inhalation reaches the lower respiratory tract, and the rest is deposited in the upper respiratory tract and in the mouth and then swallowed. As a result, some amount of inhaled fenoterol enters the gastrointestinal tract. After inhalation of a metered dose aerosol, the absolute bioavailability of fenoterol is 18.7% of the administered dose. Absorption from the lungs is biphasic - 30% of fenoterol hydrobromide is rapidly absorbed with a half-life of 11 minutes, and 70% is absorbed slowly with a half-life of 120 minutes.
Cmax of the drug in blood plasma (Cmax 45.3 pg/ml) was observed 15 minutes after a single inhalation of 100 mcg of fenoterol using a metered-dose inhaler with freon in patients with bronchial asthma. However, in studies involving healthy volunteers, in which blood tests were taken more frequently, it was found that serum Cmax of the drug was achieved earlier: 2 and 3.5 minutes after dosing. Cmax of the drug in serum after inhalation of a single dose of fenoterol 200 mcg using a tetrafluoroethane (HFA) metered-dose inhaler:
- Cmax 6.9 pg/ml, tmax15 minutes.
After oral administration, the degree of absorption is 60% of the administered dose of fenoterol hydrobromide. This amount undergoes extensive first-pass metabolism, resulting in a bioavailability of approximately 1.5%. Thus, the ingested portion of the active substance has only a minor effect on the plasma concentration after inhalation.
Distribution
Fenoterol is distributed throughout the body. Vd in a stable state after intravenous administration (Vss) is 1.9–2.7 l/kg. The distribution of fenoterol in blood plasma after intravenous administration occurs according to a three-phase pharmacokinetic model. T1/2 are tα= 0.2 minutes, tβ= 14.3 minutes and tγ= 3.2 hours. Plasma protein binding ranges from 40 to 55%.
Metabolism
The biotransformation of fenoterol hydrobromide in humans occurs through conjugation with sulfates. Following oral administration, fenoterol is metabolized primarily through sulfation. This metabolic inactivation of the parent substance begins already in the intestinal walls.
Removal
Biotransformation, including biliary excretion, is due mainly (approximately 85%) to the average total clearance of 1.1-1.8 l/min. after intravenous administration. Renal excretion of fenoterol (0.27 l/min) corresponds to approximately 15% of the average total clearance of the systemically available dose. Considering the part of the drug that binds to plasma proteins, the renal clearance value indicates tubular secretion of fenoterol in addition to glomerular filtration.
After oral and IV administration, the total radioactivity excreted in urine is approximately 39% and 65% of the dose, and the total radioactivity excreted in feces is 40.2% and 14.8% of the dose over 48 hours, respectively. After oral administration, 0.38% of the dose is excreted unchanged into the urine, while with intravenous administration - 15%. After inhalation using a metered dose inhaler, 2% of the dose is excreted unchanged in the urine within 24 hours.
In unchanged form, fenoterol hydrobromide can cross the placental barrier and enter breast milk.
The metabolism of fenoterol hydrobromide in diabetes has not been sufficiently studied.
Berotec, 1 piece, 20 ml, 1 mg/ml, solution for inhalation
Inhalation.
Solution for inhalation.
For adults and children over 12 years old,
to relieve an attack of bronchial asthma
- 0.5 ml (0.5 mg - 10 drops), in severe cases - 1-1.25 ml (1-1.25 mg - 20-25 drops) , in extremely severe cases (under medical supervision) - 2 ml (2 mg - 40 drops).
Prevention of physical exertion asthma and symptomatic treatment of bronchial asthma and chronic obstructive pulmonary disease
- 0.5 ml (0.5 mg - 10 drops) up to 4 times a day.
Children 6–12 years old (body weight 22–36 kg) to relieve an attack of bronchial asthma
- 0.25-0.5 ml (0.25-0.5 mg - 5-10 drops), in severe cases - 1 ml (1 mg - 20 drops), in extremely severe cases (under medical supervision) - 1 .5 ml (1.5 mg - 30 drops).
Prevention of exercise asthma and symptomatic treatment of bronchial asthma and other conditions with reversible narrowing of the airways
- 0.5 ml (0.5 mg - 10 drops) up to 4 times a day. Children under 6 years of age (body weight less than 22 kg) (only under medical supervision) - about 50 mcg/kg per dose (0.25-1 mg - 5-20 drops) up to 3 times a day.
The recommended dose is diluted with saline immediately before use to a volume of 3–4 ml. The dose depends on the method of inhalation and the quality of the spray. If necessary, repeated inhalations are carried out at intervals of at least 4 hours.
Aerosol.
Acute attack of bronchial asthma
- 1 dose; if necessary, inhalation can be repeated after 5 minutes. The next prescription of the drug is possible no earlier than 3 hours later. If there is no effect and additional inhalations are required, you should immediately seek medical help at the nearest hospital.
Prevention of exercise asthma and symptomatic treatment of bronchial asthma and other conditions accompanied by reversible narrowing of the airways
- 1-2 doses per 1 dose, but not more than 8 doses per day.
To obtain maximum effect, it is necessary to use a dosed aerosol correctly.
Before using the metered-dose aerosol for the first time, shake the can and press the bottom of the can twice.
Each time you use a metered dose aerosol, the following rules must be observed:
1. Remove the protective cap.
2. Take a slow, deep breath.
3. Hold the balloon and wrap your lips around the tip. The cylinder should be pointing upside down.
4. While inhaling as deeply as possible, simultaneously quickly press the bottom of the balloon until one inhalation dose is released. Hold your breath for a few seconds, then remove the tip from your mouth and exhale slowly. Repeat steps to receive the second inhalation dose.
5. Put on the protective cap.
6. If the aerosol can has not been used for more than 3 days, before use, press the bottom of the can once until a cloud of aerosol appears.
The cylinder is designed for 200 inhalations. After this, the cylinder should be replaced. Although some contents may remain in the canister, the amount of drug released during inhalation may be reduced.
The cylinder is opaque, so the amount of drug in the cylinder can only be determined in the following way: by removing the protective cap, the cylinder is immersed in a container filled with water. The amount of the drug is determined depending on the position of the cylinder in the water.
The tip should be kept clean and can be washed in warm water if necessary. After using soap or detergent, rinse the handpiece thoroughly with clean water.
Warning:
The plastic mouth adapter is designed specifically for the Berotec N metered aerosol and serves for precise dosing of the drug. The adapter must not be used with other metered aerosols. You also cannot use metered tetrafluoroethane-containing aerosol Berotek N with any other adapters other than the adapter supplied with the cylinder.
The contents of the cylinder are under pressure. The cylinder must not be opened or exposed to temperatures above 50 °C.
Berotec®
Treatment with BEROTEK® is carried out by inhalation using commercially available nebulizers. Pulmonary deposition and systemic bioavailability of the drug depend on the nebulizer used and may be higher than when using Berotec® N metered aerosol. When using a stationary oxygen source, the solution is best inhaled at a flow rate of 6-8 l/min.
When dosing, it should be taken into account that 20 drops equal 1 ml, with 1 drop containing 50 mcg of fenoterol hydrobromide.
The recommended dose of BEROTEK® is diluted in the nebulizer chamber with 0.9% sodium chloride solution to a final volume of 3-4 ml and inhaled until sufficient relief of symptoms is achieved. BEROTEK® must not be diluted with distilled water. The solution is diluted each time immediately before use; the remainder of the prepared solution is poured out.
BEROTEK® solution can be inhaled simultaneously with anticholinergic and mucolytic drugs for which compatibility has been proven - Atrovent (ipratropium bromide) and Lazolvan (ambroxol) inhalation solutions.
Treatment with BEROTEK® should be initiated and carried out under the supervision of medical personnel, for example, in a clinic setting.
Treatment at home may be recommended to patients after consultation with a physician in cases where the use of a low-dose metered-dose aerosol of a fast-acting beta-agonist bronchodilator (such as Berotec® N) has not been sufficient to relieve the condition. It may also be recommended for patients who require nebulizer therapy for other reasons, such as problems with the use of metered-dose aerosols or the need for higher doses.
Treatment should usually begin with the minimum recommended doses. The dose should be individualized based on the patient's needs and adjusted based on the severity of the acute episode. The drug should be discontinued when sufficient relief of symptoms is achieved.
If necessary, the dose can be reapplied after at least 4 hours.
The dose may depend on the method of inhalation and the characteristics of the nebulizer used. The duration of inhalation can be controlled by the volume of drug dilution.
The following dosage regimens are recommended:
Adults (including patients over 75 years of age) and adolescents over 12 years of age:
a) Attacks of bronchial asthma and other conditions with reversible airway obstruction
Inhalation.
- 0.5 ml (10 drops = 500 mcg fenoterol hydrobromide) is in most cases sufficient for immediate relief of symptoms; if it is necessary to re-prescribe the drug up to 4 times a day, a reduction in individual doses should be considered depending on the effectiveness of the nebulizer;
- in severe cases (for example, for most patients admitted to the intensive care unit), higher doses may be required - 1-1.25 ml (20-25 drops = 1000-1250 mcg of fenoterol hydrobromide);
- in extremely severe cases, under the supervision of a physician, doses of up to 2 ml (40 drops = 2000 mcg of fenoterol hydrobromide) can be administered;
b) Prevention of attacks of bronchial asthma due to physical stress
Inhalation.
0.5 ml (10 drops = 500 mcg fenoterol hydrobromide) before physical activity.
Children from 6 to 12 years old (with a body weight of about 22-36 kg):
a) Attacks of bronchial asthma and other conditions with reversible airway obstruction:
Inhalation.
- 0.25-0.5 ml (5-10 drops = 250-500 mcg fenoterol hydrobromide) is in most cases sufficient for immediate relief of symptoms;
- if it is necessary to re-prescribe the drug up to 4 times a day, a reduction in individual doses should be considered depending on the effectiveness of the nebulizer; in severe cases (for example, in most cases of treatment in a hospital setting) higher doses of up to 1 ml (20 drops = 1000 mcg fenoterol hydrobromide) may be required;
- in extremely severe cases, under the supervision of a physician, doses of up to 1.5 ml (30 drops = 1500 mcg of fenoterol hydrobromide) can be administered;
b) Prevention of attacks of bronchial asthma due to physical stress:
Inhalation.
0.5 ml (10 drops = 500 mcg fenoterol hydrobromide) before physical activity;
Children under 6 years of age (weight less than 22 kg):
Due to the limited information on the use of the drug in this age group, treatment is carried out only under the supervision of a physician, prescribing the drug in the following dose: inhalation of about 50 mcg of fenoterol hydrobromide per dose (= 0.05 ml or 1 drop) per 1 kg of body weight, but no more than 0.5 ml (10 drops) per dose up to 3 times a day.
BEROTEK N
Directions for use and doses
Doses for adults and adolescents over 12 years of age
Attacks of bronchial asthma and other conditions accompanied by reversible airway obstruction
In most cases, one inhalation dose is sufficient to relieve bronchospasm; If breathing relief does not occur within 5 minutes, inhalation can be repeated.
If there is no effect after two inhalations and additional inhalations are required, you should immediately seek medical help at the nearest hospital. Prevention of asthma by physical effort
1-2 inhalation doses before physical activity, up to 8 inhalations per day.
Doses for children from 6 to 12 years
Attacks of bronchial asthma and other conditions accompanied by reversible airway obstruction
In most cases, one inhalation dose is sufficient to relieve bronchospasm; If breathing relief does not occur within 5 minutes, inhalation can be repeated.
If there is no effect after two inhalations and additional inhalations are required, you should immediately seek medical help at the nearest hospital. Prevention of asthma by physical effort
1-2 inhalation doses before physical activity, up to 8 inhalations per day.
Doses for children from 4 to 6 years
Due to limited experience with children under 6 years of age, the drug should be used only as directed by a physician and under adult supervision.
Attacks of bronchial asthma and other conditions accompanied by reversible airway obstruction
To relieve bronchospasm, one inhalation dose is sufficient.
If there is no effect, you should immediately seek medical help at the nearest hospital.
Prevention of asthma by physical effort
1 inhalation dose before physical activity, up to 4 inhalations per day.
Mode of application
To achieve maximum effect, it is necessary to use a dosed aerosol correctly.
Before using metered dose aerosol for the first time, press the bottom of the can twice.
Each time you use a metered dose aerosol, the following rules must be observed:
1. Remove the protective cap.
2. Exhale slowly and completely.
3. Hold the can as shown in Fig. 1 and tightly wrap your lips around the tip. In this case, the arrow and the bottom of the inhaler are facing upward.
4. While inhaling as deeply as possible, simultaneously quickly press the bottom of the can until the inhalation dose is released. Hold your breath for a few seconds, then remove the mouthpiece from your mouth and exhale slowly.
If repeated inhalation is required, repeat the same steps (steps 2-4).
5. Put on the protective cap.
6. If the aerosol can has not been used for more than three days, press the bottom of the can once before use.
The cylinder is designed for 200 inhalations. After this, the cylinder should be replaced. Although some drug may remain in the canister, the amount of drug released during inhalation may be reduced. The cylinder is opaque, so the amount of drug in the cylinder can only be determined in the following way: by removing the protective cap, the cylinder is immersed in a container filled with water. The amount of the drug is determined depending on the position of the cylinder in the water (see Fig. 2).
The inhaler should be washed at least once a week.
It is important to keep the mouthpiece of your inhaler clean so that medication does not accumulate and block the spray.
To clean, first remove the dust cap and remove the container from the inhaler. Rinse the inhaler with warm water to remove any accumulated medication and/or visible dust (see Figure 3).
After cleaning, shake the inhaler and allow it to air dry without using heating devices. When the mouthpiece is dry, return the container and dust cap to their place (see Fig. 4).
WARNING: The plastic mouthpiece is designed specifically for Berotek® N and is used for precise dosing of the drug. The mouthpiece should not be used with other metered dose aerosols. Also, Berotec® N should not be used with any adapters other than the mouthpiece supplied with the drug.
The contents of the cylinder are under pressure. The container must not be opened or heated above 50°C.
